Drug intelligence / Profile preview

OPB-111077 + bendamustine

Development stage
Phase 1
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**OPB-111077 + bendamustine** is an experimental combination drug therapy under investigation for the treatment of relapsed or refractory diffuse large B-cell lymphoma (DLBCL). OPB-111077 is a first-in-class, orally administered small molecule that inhibits mitochondrial oxidative phosphorylation (OXPHOS), thereby disrupting the energy metabolism of cancer cells[6][8]. Bendamustine is a cytotoxic alkylating agent that causes DNA crosslinking and cell death[6][8]. Preclinical and early clinical data suggest a synergistic antitumor effect when OPB-111077 is combined with bendamustine: bendamustine reprograms lymphoma cells toward OXPHOS dependence, making them more susceptible to OPB-111077-mediated inhibition of mitochondrial respiration[6]. The combination is being evaluated primarily for its safety, tolerability, and preliminary efficacy in patients with relapsed or refractory DLBCL who have received prior therapies and are not eligible for curative treatment[1][2][6][7][8]. OPB-111077 is developed by Otsuka Pharmaceutical.

02

Targets

DNAND1 (Mitochondrial electron transport chain complex I)STAT3 (Signal Transducer and Activator of Transcription 3)

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